177469-96-4
基本信息
Unii-Q70OH404hr
Implitapide [inn]
2(S)-Cyclopentyl-2-[4-(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-ylmethyl)phenyl]-N-[2-hydroxy-1(R)-phenylethyl]acetamide
(2S)-2-cyclopentyl-2-[3-[(2,4-dimethylpyrido[2,3-b]indol-9-yl)methyl]phenyl]-N-[(1R)-2-hydroxy-1-phenylethyl]acetamide
Benzeneacetamide, α-cyclopentyl-4-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]-N-[(1R)-2-hydroxy-1-phenylethyl]-, (αS)-
(alphaS)-alpha-Cyclopentyl-4-[(2,4-dimethyl-9H-pyrido[2,3-b]indol-9-yl)methyl]-N-[(1R)-2-hydroxy-1-phenylethyl]benzeneacetamide
物理化学性质
沸点 | 742.9±60.0 °C(Predicted) |
密度 | 1.21±0.1 g/cm3(Predicted) |
储存条件 | -20°C储存 |
溶解度 | 溶于二甲基亚砜 |
酸度系数(pKa) | 14.22±0.10(Predicted) |
形态 | Solid |
颜色 | White to off-white |
常见问题列表
MTP
Implitapide suppresses MTP activity using a recombinant human form complexed with protein disulphide isomerase (IC 50 =10 nM) and inhibit secretion of apoB-containing very low-density lipoprotein (VLDL)-like lipoproteins from a human hepatoma cell (HepG2) with an IC 50 value of 1.1 nM.
Implitapide (3.2 mg/kg/d) significantly reduces the plasma lipid levels to nearly or below the chow diet (CD) level at 4 and 8 weeks of treatment (p<0.01). Implitapide (3.2 mg/kg/d) markedly suppresses lipid-stained lesions in the mice fed the western-type diet (WD). Implitapide (3.2 mg/kg/d) significantly decreases lesion area by 83% compared with that of the WD group (p<0.01). ApoE KO mice fed a WD containing Implitapide (1, 5, and 15 mg/kg/d) for 14 weeks have been shown to reduce significantly both plaque area (by 66, 78, and 93%, respectively) and lipid moieties within plaque (4.3, 2.6, and 0%, respectively, versus 9.5% in controls). Implitapide at a dosage of approximately 3.2 mg/kg/d significantly reduces the lipid-stained aortic lesions by 83% in apoE KO mice.